Azelastine hydrochloride

Azelastine hydrochloride Basic information
Product Name:Azelastine hydrochloride
Synonyms:a5610;azeptin;e-0659;w-2979m;AZELASTINE HYDROCHLORIDE;4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)-phthalazin-1-one hydrochloride;4-[(4-Chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone Hydrochloride;Allergodil
CAS:79307-93-0
MF:C22H25Cl2N3O
MW:418.36
EINECS:620-469-0
Product Categories:Antihistaminic;Astelin;Intermediates & Fine Chemicals;Pharmaceuticals;Histamine receptor
Mol File:79307-93-0.mol
Azelastine hydrochloride Structure
Azelastine hydrochloride Chemical Properties
Melting point 225--2290C
storage temp. Inert atmosphere,Store in freezer, under -20°C
solubility DMSO: >10mg/mL
form powder
color white to off-white
Merck 14,906
Stability:Incompatible with strong oxidizing agents.
InChIInChI=1S/C22H24ClN3O.ClH/c1-25-13-4-5-18(12-14-25)26-22(27)20-7-3-2-6-19(20)21(24-26)15-16-8-10-17(23)11-9-16;/h2-3,6-11,18H,4-5,12-15H2,1H3;1H
InChIKeyYEJAJYAHJQIWNU-UHFFFAOYSA-N
SMILESC1(=O)C2=C(C=CC=C2)C(CC2=CC=C(Cl)C=C2)=NN1C1CCCN(C)CC1.[H]Cl
CAS DataBase Reference79307-93-0(CAS DataBase Reference)
Safety Information
Hazard Codes Xn
Risk Statements 22
RTECS TH9203900
HS Code 2933992600
ToxicityLD50 in male, female mice, male, female rats (mg/kg): 36.5, 35.5, 26.9, 30.3 i.v.; 56.4, 42.8, 43.2, 46.6 i.p.; 63.0, 54.2, 66.5, 59.6 s.c.; 124, 139, 310, 417 orally (Zechel)
MSDS Information
Azelastine hydrochloride Usage And Synthesis
DescriptionAzelastine hydrochloride is an orally effective antihistamine useful in the treatment of asthma and nasal allergy. It appears to inhibit release of histamine, in addition to antagonizing its action.
Chemical PropertiesWhite or almost white, crystalline powder.
OriginatorAsta-Werke(Degussa) (W. Germany)
UsesOrally active H1-hystamine receptor antagonist. Antihistaminic
DefinitionChEBI: The hydrochloride salt of azelastine.
Brand nameAstelin (Medpointe); Optivar (Medpointe);AZEPTIN.
General Description(±)-4-[(4-chlorophenyl)methyl]-2-(hexahydro-l-methyl-1H-azepin-4-yl)-l-(2H)-phthalazinone monohydrochloride (Optivar), is a whitecrystalline powder that is sparingly soluble in water,methanol, and propylene glycol and slightly soluble inethanol, octanol, and glycerine. The commercial preparationis available as a 0.05% sterile ophthalmic solution fortopical administration to the eyes. Each milliliter of azelastinesolution contains 0.5-mg azelastine hydrochlorideequivalent to 0.457 mg of azelastine base, the preservativebenzalkonium chloride (0.125 mg), and inactive ingredientsincluding disodium edetate dihydrate, hydroxypropylmethylcellulose,sorbitol solution, sodium hydroxide, andwater for injection. The solution has a pH of approximately5.0 to 6.5 and an osmolality of approximately 271to 312 mOsm/L.
The recommended dose of azelastine solution is 1 dropinstilled into each affected eye twice a day. This drugproduct is for ocular administration only and not for injectionor oral use. Absorption of azelastine following ocularadministration is relatively low (less than 1 ng/rnL).Absorbed drug undergoes extensive oxidative N-demethylationby CYP, and the parent drug and metabolite are eliminatedprimarily in the feces. The most frequently reportedadverse reactions are transient eye burning or stinging,headaches, and bitter taste. Azelastine solution should beused with caution during pregnancy or while nursing, becauseits safety has not been studied under these circumstances.
Biochem/physiol ActionsH1 histamine receptor antagonist; NF-kB activator.
Safety ProfilePoison by ingestion andintravenous routes. An experimental teratogen. Otherexperimental reproductive effects. When heated todecomposition it emits toxic fumes of NOx and HCl.
Azelastine hydrochloride Preparation Products And Raw materials
Preparation Products2-Tetralin-1-yl-4,5-dihydro-1H-imidazole hydrochloride
AZELASTINE HYDROCHLORIDEIMP. E (EP) Z-ISOMER: (Z)-3-(4-CHLOROBENZYLIDENE)-ISOBENZOFURAN-1(3H)-ONE Methyl Topotecan hydrochloride AZELASTINE HYDROCHLORIDEIMP. D (EP): 4-(4-CHLOROBENZYL)PHTHALAZIN-1(2H)-ONE Phenylacetone Sibutramine hydrochloride Tramadol hydrochloride AZELASTINE HCL IMP. A (EP): BENZOYLDIAZANE (BENZOHYDRAZIDE) AZELASTINE HYDROCHLORIDE IMP. B (EP) AS HYDROCHLORIDE: 1-BENZOYL-2-[(4RS)-1-METHYLHEXAHYDRO-1H-AZEPIN-4-YL]DIAZANEHYDROCHLORIDE AZELASTINE HYDROCHLORIDE IMP. C (EP): 2-[(4-CHLOROPHENYL)ACETYL]BENZOIC ACID AZELASTINE HYDROCHLORIDE MM STANDARD DIBENZYLTOLUENE Azelastine hydrochloride AZELASTINE HYDROCHLORIDE EP STANDARD azelastine hydrochloride Azelastine Hydrochloride IMpurity D Azelastine Impurity 1 HCl 4-(4-CHLOROBENZYL)-2-(2-(1-METHYLPYRROLIDIN-2-YL)ETHYL)PHTHALAZIN-1(2H)-ONE

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